COMPOUNDS WITH SPIRO AND AROMATIC RINGS AND APPLICATION THEREOF Russian patent published in 2022 - IPC C07D471/04 A61K31/4985 A61K31/519 A61P35/00 A61P35/02 A61P43/00 C07D487/04 C07D519/00 

Abstract RU 2781100 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound by the formula I, or to a pharmaceutically acceptable salt, or enantiomer, or tautomer thereof; wherein X1 and X2 are independently selected from a bond or CRaRb; X3 constitutes S; X4 is selected from N or CRc, and Ra, Rb, and Rc are independently selected from H, an unsubstituted C1-6alkyl, or an unsubstituted C1-6alkoxyl; R1, R2, R3, R4, and R7 are independently selected from H, an unsubstituted C1-6alkyl, or an unsubstituted C1-6alkoxyl; ring A is selected from a substituted or unsubstituted C5-6aryl, or a substituted or unsubstituted 5-6-membered heteroaryl, wherein the heteroaryl contains 1 or 2 heteroatoms selected from the following atoms: N or S; ring C is selected from a substituted or non-substituted 9-membered bicyclic heterocyclyl, a substituted or unsubstituted C5-6 monocyclic aryl, a substituted or unsubstituted 5-6-membered monocyclic heteroaryl, or a substituted or unsubstituted 9-membered bicyclic heteroaryl, wherein the heterocyclyl or heteroaryl contains 1-4 heteroatoms selected from the following atoms: N, O, or S; R5 and R6 are independently selected from H, -OH, a halogen, a cyano, a substituted or unsubstituted amino, a substituted or unsubstituted C1-6alkyl, or an unsubstituted C1-6alkoxyl; n constitutes any integer from 0 to 3; and wherein the term “substituted” relates to one or more hydrogen atoms in the group, substituted with a substitute selected from: halogen, -OH, -NH2, -NH(unsubstituted C1-6alkyl), -CN, a halogenated C1-8alkyl, an unsubstituted C1-8alkoxyl. Also proposed is a method for producing the compound by the formula I.

EFFECT: compound by the formula I has a higher inhibitory activity against SHP2 and, thus, can be applied to prevent or treat an SHP2-associated disease.

21 cl, 4 tbl, 23 ex

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RU 2 781 100 C1

Authors

Zheng, Qiangang

Xu, Ming

Zeng, Qinglong

Li, Jing

Zhuge, Hao

Dates

2022-10-05Published

2019-11-05Filed